Log P analyzation-based discovery of GSH activated biotin-tagged fluorescence probe for selective colorectal cancer imaging.

Targeted activatable fluorescent probes could provide an effective approach for colorectal cancer imaging. In this study, F1 was found as an effective targeted activatable fluorescent probe based on log P analysis. In vitro experiments demonstrated that the initial fluorescence of the developed probe F1 was initially well quenched, and the fluorescence increased after the probe interacted with glutathione. Cell imaging results showed that the probe had good cell permeability and selectivity. Remarkably, F1 displayed enhanced tumor tissue fluorescence in MC-38 tumor-bearing mice. Notably, it showed selectivity in imaging clinical specimens of human colorectal cancer tissues. Accordingly, this study shows that log P analysis can facilitate the developing efficient of biotin-tagged activatable probes, and the identified F1 has a good potential in clinical colorectal cancer diagnosis. [Display omitted] • The fluorescence signal after F1 activation can be enhanced 67-fold. • F1 was found as an effective targeted activatable fluorescent probe. • F1 showed selectivity in imaging the clinical specimens of human CRC tissues. • The potential utility of log P analysis in biotin-tagged activatable probes design. [ABSTRACT FROM AUTHOR]